Design, synthesis and evaluation of antitumor and antiviral activities of 5-amino-1H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-ones (8-azaguanines) and 7-amino-1H-[1,2,3]triazolo[4,5-d]pyrimidin-5(4H)-ones (8-azaisoguanines).

[摘要]：Prepn. of 5-amino-1H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-ones and 7-amino-1H-[1,2,3]triazolo[4,5-d]pyrimidin-5(4H)-ones was accomplished by nitrosative cyclization of appropriate 2,5,6-triamino- and 4,5,6-triaminopyrimidines, resp., with HNO2. The 5-amino compds. were also prepd. by nucleophilic replacement of the methylthio group of 5-methylthio-1H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-one by appropriate amines. Similarly, some 7-amino derivs. were synthesized by replacement of the thiol groups of a 7-thiol deriv. by appropriate amines. Antitumor and antiviral activities of the synthesized compds. were evaluated in vitro.

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